Effects of mavacamten on Ca2+-sensitivity of contraction as sarcomere
length varied in human myocardium
Abstract
Background and Purpose: Heart failure can reflect impaired contractile
function at the myofilament level. In healthy hearts, myofilaments
become more sensitive to Ca2+ as cells are stretched. This represents a
fundamental property of myocardium that contributes to the
Frank-Starling response, although the molecular mechanisms underlying
the effect remain unclear. Mavacamten is a drug that binds to myosin,
which is under investigation as a potential therapy for cardiovascular
disease. We tested how mavacamten affects the sarcomere-length
dependence of Ca2+-sensitive isometric contraction to determine how
mavacamten might modulate the Frank-Starling mechanism. Experimental
Approach: Multicellular preparations from the left ventricular free wall
of hearts procured from organ donors were chemically permeabilized and
Ca2+-activated in the presence or absence of 0.5 μM mavacamten at 1.9 or
2.3 µm sarcomere length (37°C). Isometric force and frequency-dependent
viscoelastic myocardial stiffness measurements were made. Key Results:
At both sarcomere lengths, mavacamten reduced maximal force and
Ca2+-sensitivity of contraction. In the presence and absence of
mavacamten, Ca2+-sensitivity of force increased as sarcomere length
increased. This suggests that the length-dependent activation response
was maintained in human myocardium, even though mavacamten reduced
Ca2+-sensitivity. There were subtle effects of mavacamten reducing force
values under relaxed conditions (pCa 8.0), as well as slowing myosin
cross-bridge recruitment and speeding cross-bridge detachment under
maximally activated conditions (pCa 4.5). Conclusion and Implications:
Mavacamten did not eliminate sarcomere length-dependent increases in the
Ca2+-sensitivity of contraction in myocardial strips from organ donors
at physiological temperature. Pharmaceuticals that modulate myofilament
function may be useful therapies for cardiovascular disease.